Journal
CHEMMEDCHEM
Volume 6, Issue 7, Pages 1238-1248Publisher
WILEY-BLACKWELL
DOI: 10.1002/cmdc.201100085
Keywords
angelicin heteroanalogues; antitumor agents; apoptosis; photochemotherapeutic agents; pyrrolo[3,2-h]quinazolines
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Funding
- Ministero dell'Istruzione dell'Universite della Ricerca
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Heteroanalogues of angelicin, pyrrolo[3,2-h]quinazolines, were synthesized with the aim of obtaining new potent photochemotherapeutic agents. Many derivatives caused a significant decrease in cell proliferation in several human tumor cell lines after irradiation with UVA light (GI(50) = 15.2-0.2 mu m). Their phototoxicity effected apoptosis in Jurkat cells with the involvement of mitochondria (as determined by the loss of mitochondrial membrane potential and production of reactive oxygen species) and lysosomes. The phototoxicity of these compounds could be explained by lipid peroxidation.
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